title: Synthesis, antiproliferative and mitochondrial impairment activities of bis-alkyl-amino transplatinum complexes.
abstract: A convenient synthetic route and the characterization of complexes trans-[PtCl2(L)(PPh3)] (L=Et2NH (2), (PhCH2)2NH (3), (HOCH2CH2)2NH) (4) are reported. The antiproliferative activity was evaluated on three human tumor cell lines. The investigation on the mechanism of action highlighted for the most active complex 4 the capacity to affect mitochondrial functions. In particular, both the induction of the mitochondrial permeability transition phenomenon and an aspecific membrane damage occurred, depending on concentration.
authors.affiliation: Department of Pharmaceutical and Pharmacological Sciences, University of Padova, Via F. Marzolo 5, 35131 Padova, Italy. Electronic address: lisa.dallavia@unipd.it.
authors.forename: Lisa
authors.initials: L
authors.lastname: Dalla Via
authors.forename: Aída N
authors.initials: AN
authors.lastname: García-Argáez
authors.forename: Arianna
authors.initials: A
authors.lastname: Adami
authors.forename: Silvia
authors.initials: S
authors.lastname: Grancara
authors.forename: Pamela
authors.initials: P
authors.lastname: Martinis
authors.forename: Antonio
authors.initials: A
authors.lastname: Toninello
authors.forename: Daniela
authors.initials: D
authors.lastname: Belli Dell'Amico
authors.forename: Luca
authors.initials: L
authors.lastname: Labella
authors.forename: Simona
authors.initials: S
authors.lastname: Samaritani
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D056831:Coordination Complexes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006367:HeLa Cells; D006801:Humans; D007536:Isomerism; D053078:Membrane Potential, Mitochondrial / Q000187:drug effects; D008928:Mitochondria / Q000187:drug effects* / Q000378:metabolism; D010720:Phosphines / Q000737:chemistry; D010984:Platinum / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D056831:Coordination Complexes; D010720:Phosphines; D010984:Platinum
keywords: Antiproliferative activity; Mitochondria; Mitochondrial permeability transition; Oxidative stress; Transplatinum complexes